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已发表论文

本文章已被撤回:甲氨蝶呤 (Methotrexate) 缀合、聚醚基聚合物胶束在对富含叶酸 (folate) 受体的肿瘤治疗中的疗效

 

Authors Chen YZ, Zhang W, Huang YK, Gao F, Sha XY, Lou KY, Fang XL

Published Date June 2015 Volume 2015:10 Pages 4043—4057

DOI http://dx.doi.org/10.2147/IJN.S79045

Received 10 December 2014, Accepted 29 March 2015, Published 19 June 2015

Approved for publication by Dr Lei Yang

***本文章已被撤回***



Abstract: The therapeutic effect of methotrexate (MTX)-conjugated Pluronic-based polymeric mixed micelles (F127/P105-MTX) on the folate receptor-overexpressing tumors treatment was investigated in this study. Due to its high structural similarity to folic acid and the high expression of folate receptor in most solid tumors, MTX serves as not only a cytotoxic agent but also a homing ligand. Cellular uptake and the endocytic mechanism studies of MTX-conjugated mixed micelles were performed in folate receptor-rich KBv and folate receptor-deficient A-549 cancer cells. Additionally, the efficacy and safety studies of F127/P105-MTX in KBv tumor-bearing mice were evaluated. Results indicate that F127/P105-MTX significantly enhanced the cellular uptake in KBv cells as compared to that of conventional non-MTX-conjugated mixed micelles. Moreover, the results showed that F127/P105-MTX can be internalized by both caveolae- and clathrin-mediated endocytosis in energy-dependent and folate receptor-dependent manners. The in vitro and in vivo antitumor efficacies of F127/P105-MTX were significantly enhanced in comparison with MTX-entrapped mixed micelles. Furthermore, no acute toxicities to hematological system and major organs have been observed after intravenous administration during the regimen. Therefore, our results suggest that F127/P105-MTX could be an effective and safe nano-drug delivery system for cancer therapy, especially for the folate receptor-rich cancer treatment.
Keywords: methotrexate-conjugated, mixed micelles, folate receptor, Pluronic, KBv cells

Keywords: methotrexate-conjugated, mixed micelles, folate receptor, Pluronic, KBv cells